BM0033 Sigma-Aldrich


≥98% (HPLC)

Synonym: (S)-5-Chloro-1-(1-cyclopropylethyl)-3-(2,6-dichloro-4-(difluoromethoxy)phenylamino)-pyrazin-2(1H)-one, 5-Chloro-1-[(1S)-1-cyclopropylethyl]-3-[[2,6-dichloro-4-(difluoromethoxy)phenyl]amino]-2(1H)-pyrazinone

  • CAS Number 1173435-64-7

  • Empirical Formula (Hill Notation) C16H14Cl3F2N3O2

  • Molecular Weight 424.66

  •  MDL number MFCD28977961



Related Categories B, Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, Cell Signaling and Neuroscience,
Quality Level   100
assay   ≥98% (HPLC)
form   powder
optical activity   [α]/D +16 to +21°, c = 0.4 in chloroform-d
color   white to light brown
solubility   DMSO: 20 mg/mL, clear
storage temp.   room temp
SMILES string   ClC1=CC(OC(F)F)=CC(Cl)=C1NC2=NC(Cl)=CN([C@@H](C)C3CC3)C2=O



5, 25 mg in glass bottle

Biochem/physiol Actions

BMS-665053 is a pyrazinone-containing antagonist that targets corticotropin-releasing factor/hormone (CRF or CRH) receptor 1 (CRF1, CRF-R1, CRFR-1, CRH-R1, CRHR-1) with high affinity (IC50 </= 1.0 nM against 150 pM ovine CRF for binding human and rat CRF-R1), potency (IC50 = 4.9 nM against 1 nM CRF-stimulated cAMP production in human Y-79 retinoblastoma cells), and selectivity, displaying no affinity toward CRF-R2/CRF2 (IC50 >10 μM against 150 pM ovine CRF in binding assay). BMS-665053 exhibits anxiolytic efficacy in a defensive withdrawal anxiety test in rats in vivo (10 mg/kg p.o.) with good oral bioavailability (F = 52%).

Features and Benefits

BMS-665053 is available through a partnership with Bristol-Myers Squibb (BMS). To learn more and view other BMS compounds, visit

Legal Information

Sold for research purposes only under agreement from BMS.

Safety & Documentation

Safety Information

NONH for all modes of transport


Certificate of Analysis (COA)

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